肝细胞受体显像剂^(99)Tc^m-GSA的制备及其药盒化  

The Preparation of ^(99)Tc^m-GSA and Its Instant Lyophilized Kit for Hepatic Receptor Imaging

作　　者：毛一雷[1] 董一女[1] 杨文江[2] 张现忠[2] 唐志刚[2] 王学斌[2] 

机构地区：[1]中国医学科学院中国协和医科大学北京协和医院肝脏外科,北京100730 [2]放射性药物教育部重点实验室北京师范大学化学学院,北京100875

出　　处：《同位素》2008年第2期88-94,128,共8页Journal of Isotopes

基　　金：美国中华医学基金会(China Medical Board of New York;CMB)基金资助(06-837)

摘　　要：合成了二乙烯三胺五乙酸-半乳糖基人血清白蛋白(Diethylenetriamine Pentaacetic Acid-galactosyl-hu-man Serum Albumin,GSA),对其进行了99Tcm标记;进一步研制了无菌GSA一步法冻干药盒,并观察了99Tcm-GSA在正常小鼠以及肝损伤模型小鼠中的生物分布。标记结果显示,99Tcm-GSA的标记率>96%。生物分布结果显示,99Tcm-GSA在正常小鼠肝脏中有较高的摄取,在30 min时,肝脏摄取仍大于70%ID/g,且具有饱和性;在肝损伤模型中,肝摄取值低于正常小鼠(P=0.032 4)。冻干药盒法与湿法标记所得99Tcm-GSA的生物分布相当。所得GSA一步法冻干药盒标记简单可靠,并且标记后的GSA仍有优良的生物性能,可用于进一步临床研究及应用。methods. Biodistribution of 99Tcm-GSA was investigated in both normal and liver-injury model mice. 99Tcm-GSA showed high liver The ligand GSA （diethylenetriamine pentaacetic acid-galactosyl-human serum albumin） was synthesized by introducing bifunctional chelator DTPA （diethylenetriamine pentaacetic acid） to human serum albumin （HSA） via DTPA anhydride first, and then coupling galactosyl units （2-imino-2-methoxyethyl-thio-galactose） to DTPA-HSA. GSA was labeled with ^99Tc^m by using SnCl2 as reductant and the labeling conditions of ^99Tc^m-GSA were optimized. Lyophilized kit of GSA was also developed for instant preparing of %99 Tc^m- GSA. The labeling yields in excess of 96% by using both of liquid and lyophilized labeling uptake in normal mice （〉 70%ID · g^-1 at 30 min after injection）. The liver uptake in liver-injury model mice is lower than that of in normal mice （P=0. 032 4）. The promising biological properties of ^99Tc^m-GSA combined with the development of reliable and instant lyophilized GSA kit afford the opportunity of liver receptor imaging for routine clinical assessment of hepatocyte function.

关 键 词：GSA 药盒化 ^99TC^M标记 肝受体显像剂 

分 类 号：TQ463[化学工程—制药化工] R446.6[医药卫生—诊断学]